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Protease inhibitors (1 mM PMSF (fresh from 1 M stock in i-propanol), 1 μg/mL each leupeptin, aprotinin, pepstatin, 1-5 mM EDTA, 0.5-1 mM EGTA, 5 mM aminocaproic acid) or commercial protease inhibitor cocktail (use according to the manufacturer's instruction) 1 mM each Na 3 VO 4 and Na 4 P 2 O 7 as phosphatase inhibitor (if phosphorylation ...
These protease inhibitors prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles. Protease inhibitors that have been developed and are currently used in clinical practice include:
Protease inhibitors block the viral protease enzyme necessary to produce mature virions upon budding from the host membrane. Particularly, these drugs prevent the cleavage of gag and gag/pol precursor proteins. [16] Virus particles produced in the presence of protease inhibitors are defective and mostly non-infectious.
AEBSF or 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride is a water-soluble, irreversible serine protease inhibitor with a molecular weight of 239.5 Da. It inhibits proteases like chymotrypsin, kallikrein, plasmin, thrombin, and trypsin. The specificity is similar to the inhibitor PMSF, nevertheless AEBSF is more stable at low pH values ...
Tipranavir is a nonpeptidic HIV-1 protease inhibitor [11] and reached the market in 2005. [18] Unlike other HIV protease inhibitors on the market, tipranavir was developed from a nonpeptidic coumarin template and its antiprotease activity was discovered by high-throughput screening. [23]
Many naturally occurring protease inhibitors are proteins. [2] In medicine, protease inhibitor is often used interchangeably with alpha 1-antitrypsin (A1AT, which is abbreviated PI for this reason). [3] A1AT is indeed the protease inhibitor most often involved in disease, namely in alpha-1 antitrypsin deficiency.
Ubenimex (), also known more commonly as bestatin, is a competitive, reversible protease inhibitor.It is an inhibitor of arginyl aminopeptidase (aminopeptidase B), [3] leukotriene A 4 hydrolase (a zinc metalloprotease that displays both epoxide hydrolase and aminopeptidase activities), [4] alanyl aminopeptidase (aminopeptidase M/N), [5] leucyl/cystinyl aminopeptidase (oxytocinase ...
TPCK is an irreversible inhibitor of chymotrypsin. Also inhibits some cysteine proteases such as caspase, papain, bromelain or ficin. [1] It does not inhibit trypsin or zymogens. TPCK is observed covalently bound in the active site of Caspase 3 in the crystal structure of the complex solved in 2010. [2]
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